The crying game: lipid-based ophthalmic nanomedicines, and in vitro models to test their performance against dry eye disea

LETICIA HERMINIA HIGA; VICTORIA REBECA DANA GONZALES EPELBOIM ; KAJAL GHOSAL ; ANA PAULA PEREZ; ALTUBE, MARIA JULIA; MARIA JOSE MORILLA; EDER LILIA ROMERO

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY

EDITIONS SANTE

Lugar: Amsterdam ; Año: 2025

1773-2247

Dry eye disease (DED), the most prevalent ocular surface disorder worldwide, is currentlytreated with topical formulations for hydration, lubrication, or anti-inflammatory action. Due tonatural barriers of the ocular surface, which limit retention and penetration of exogenousmaterials, the local bioavailability of topical formulations is minimal. Lipid-based nanomedicinesare the most accepted nanomedicines by the pharmaceutical industry and regulatory agencies.Evaporative DED cases could benefit from topical mucoadhesive or mucopenetrating lipid-basedophthalmic nanomedicines (LBON). Besides lubricating and restoring the lipid film, topicalnanomedicines offer site-specific drug delivery, magnified targeted intracellular delivery, andreduced systemic drug distribution. The resultant reduced dosing frequency may improvepatients´ adherence to chronic treatments. To treat DED, however, LBON must not interfere withvision or irritate, and their chemical composition, osmolarity, viscosity, pH, and refractive indexmust be properly selected /adjusted. Importantly, pharmacokinetics and pharmacodynamics ofnanomedicines depend on the techniques used to produce each nanoparticulate structure.Hence, the structural features and resultant activities of nanomedicines prepared at lab scale,differ from those being manufactured at larger industrial scales. Due to ethical and economicreasons, preclinical assessment of LBON should therefore be performed using in vitro diseasemodels. Here, the preclinical performances of LBON reported over the past 10 years, are criticallyexamined. Overall, to become more significant and predictable, further preclinical developmentsof LBON need to become more technically rigorous and include the help of more sophisticatedand broadly available in vitro models